Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time.
about
Novel ubiquitin-derived high affinity binding proteins with tumor targeting properties.Target engagement and drug residence time can be observed in living cells with BRET.Translating slow-binding inhibition kinetics into cellular and in vivo effectsClozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism.Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systems.Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands.On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.The drug-target residence time model: a 10-year retrospective.Cell membranes… and how long drugs may exert beneficial pharmacological activity in vivoThe Role of Target Binding Kinetics in Drug Discovery.Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells.Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.Effects of target binding kinetics on in vivo drug efficacy: koff , kon and rebinding.Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism.Avidity and positive allosteric modulation/cooperativity act hand in hand to increase the residence time of bivalent receptor ligands.Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time.Distinct in vivo target occupancy by bivalent- and induced-fit-like binding drugs.Pharmacodynamics: Which trails are your drugs taking?Multivalency in the gas phase: H/D exchange reactions unravel the dynamic "rock 'n' roll" motion in dendrimer-dendrimer complexes.Link between a high for drug binding and a fast clinical action: to be or not to be?
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Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time.
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article científic
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article scientifique
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articol științific
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articolo scientifico
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artigo científico
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artigo científico
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artigo científico
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artikel ilmiah
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artikull shkencor
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artículo científico
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name
Rebinding: or why drugs may ac ...... n vitro target residence time.
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type
label
Rebinding: or why drugs may ac ...... n vitro target residence time.
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prefLabel
Rebinding: or why drugs may ac ...... n vitro target residence time.
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P2860
P1476
Rebinding: or why drugs may ac ...... n vitro target residence time.
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P2093
Georges Vauquelin
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P304
P356
10.1517/17460441.2010.512037
P407
P577
2010-08-17T00:00:00Z